Pharmaceutical Formulation with Improved Solubility and Bioavailability

Abstract

The present invention relates to a pharmaceutical formulation comprising at least one active pharmaceutical ingredient (API) having low aqueous solubility or a pharmaceutically acceptable salt thereof in the form of particles of a size between 1 and 800 nm, wherein said particles are encapsulated within a large microparticle of a size between 1 and 100 μm formed by a matrix comprising at least an excipient. Therefore, the API is entrapped or encapsulated in the microparticles of excipients. This pharmaceutical formulation contains the pharmaceutical active ingredient having improved solubility and subsequently supra-bioavailability.

Description

[0001]The invention relates to pharmaceutical formulations wherein one or more active pharmaceutical ingredient (API) is present in a sub-micron form to influence the solubility and bioavailability of the drug.BACKGROUND ART[0002]Most of the recent discovered pharmaceuticals present poor water solubility, leading to their low effective concentration in biofluids and poor bioavailability. Different strategies were developed to overcome this challenge, such as size reduction, modification of crystallinity, chemical alteration, solubilization in surfactant micelles or the use of pharmaceutical carriers such as polymeric micro- and nanoparticles, liposomes, solid-lipid particles, niosomes and others. Pharmaceutical carriers demonstrate a broad variety of useful properties such as longevity, targetability, intracellular penetration, reduced drug doses, which result in increased patient comfort and compliance (K. Margulis-Goshen, S. Magdassi, Nanomedicine: Nanotechnology, Biology, and Med...

AI Technical Summary

Benefits of technology

The patent text discusses the use of small particles of drugs to improve their solubility and bioavailability, which can be beneficial in treating certain medical conditions. These small particles can be easily encapsulated into larger microparticles, which can help with the formulation of pharmaceutical preparations, improve taste and shelf-life, and make handling easier. The small size of the drugs can also reduce adverse effects and food interactions, resulting in better patient compliance with the treatment.

Problems solved by technology

Most of the recent discovered pharmaceuticals present poor water solubility, leading to their low effective concentration in biofluids and poor bioavailability.

Most of the conventional techniques to produce pharmaceutical ingredients have difficulty in controlling particle size.

These processes present several drawbacks such as presence of undesirable materials in the final product (residual monomers or organic solvents), production of liquid suspensions, slow extraction rate or difficulty to scale-up the process.

However, the spray drying technique involves evaporation of the solvent using hot air.

The high temperatures employed for such processing can sometimes degrade thermally labile drugs and excipients, produce large particles with broad distribution of particles sizes, impair resolubilization and can be prone to explosion if organic or alcoholic solvents are used in which low availability drugs need be dissolved.

Additionally, the recovery and handling of sub-micron particles present several technical difficulties for industry (ISO / TR 12885:2008).

Images